Platensimycin is a novel antibiotic having a wide antimicrobial spectrum, which has been isolated from Streptomyces platensis, a kind of fungi found in the soil of South Africa by Merck Co., USA.

In the past decades, novel antibiotics kept being discovered from nature and in the laboratory. But human defense system against infection has been consistently compromised. Microbes keep developing resistance against the conventional antibiotics. Multi-drug resistant bacteria bring serious infection problems; and particularly hospital acquired (nosocomial) infection is more serious. In-patients are weak, and they are more easily infected. Once they are infected, it is very difficult to treat the infection with drugs and it might even result in death.
Therefore, development of new drugs having completely different physiological mechanisms to attack pathogens is required. Platensimycin isolated from the fungus Streptomyces platensis is one of them.
Platensimycin is a selective intracellular lipid synthesis inhibitor, which works on β-ketoacyl-(acyl-carrier-protein (ACP)) synthase I/II (FabF/B) to inhibit lipid synthesis. It was confirmed from the X-ray crystallographic studies that platensimycin targets the modified structure resulted from acylation of the lipogenic enzyme FabF/B. The mechanism of platensimycin is different from those of the conventional antibiotics being used clinically.
In the laboratory, chemists try to establish total synthesis routes to new compounds. In total synthesis, a complex compound is prepared from simple materials by using organic chemistry knowledge. For development of a new drug from a natural substance, investigation of structure-activity correlation is necessary. And then synthetic routes should be found for large scale preparation of the final target compound from less expensive starting materials. Total synthesis of platensimycin was first accomplished by Prof. Nicolau's research team at the Scripps Research Institute.
Platensimycin inhibits fatty acid synthesis in bacteria, and it possesses a broad spectrum antimicrobial activity against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE).
Platensimycin derivatives may be designed by introducing different substituents in the backbone of platensimycin itself. They are good candidates as promising antibiotics by inhibiting fatty acid synthesis in bacteria. A good scheme for efficient total synthesis of platensimycin should also allow facile preparation of wide variety platensimycin derivatives for bioassay.